JP4116687B2 - Semi-solid preparation for damaged skin repair - Google Patents
Semi-solid preparation for damaged skin repair Download PDFInfo
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- JP4116687B2 JP4116687B2 JP33539297A JP33539297A JP4116687B2 JP 4116687 B2 JP4116687 B2 JP 4116687B2 JP 33539297 A JP33539297 A JP 33539297A JP 33539297 A JP33539297 A JP 33539297A JP 4116687 B2 JP4116687 B2 JP 4116687B2
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- JP
- Japan
- Prior art keywords
- preparation
- damaged skin
- semi
- average particle
- solid preparation
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- Expired - Fee Related
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Description
【0001】
【発明の属する技術分野】
本発明は、粉末糖を配合し、硬度の経時変化が小さく、安定で、長期間良好な使用感を保つ損傷皮膚修復用半固形製剤に関する。
【0002】
【従来の技術】
糖は創傷治癒作用、肉芽形成作用を有することから火傷、開放創の治療に用いられている。また、近年では糖にポビドンヨード等の抗菌剤を加えた製剤が、損傷皮膚修復用製剤として用いられている〔R. A. Knutson et. al.; Southern Medical Journal, Vol. 74, No.11, 1329-1335(1981)及び曽根清和ら;「病院薬学」、Vol. 10, No.5, 315-322(1984)〕。
【0003】
【発明が解決しようとする課題】
しかしながら、このような糖を含有する製剤は、調製後経時的に硬度が増すという問題点があった。硬度の増加は展延性を悪化させ、傷部分への塗付を困難にする。また糖含有製剤は、経時的に均一性が失われ、ザラザラした使用感となるという問題点も有していた。
【0004】
糖含有製剤の硬度を下げる方法としては、糖の配合量を減少させたり、水の配合量を増加させる方法があるが、いずれの方法も製剤の上層又は下層に液の滲みが出たり、斑点が出現する等、安定性に問題があった。
また、最近、糖を含有する製剤の伸展性を改善するため高濃度のグリセリンを配合する方法が報告された(特開平9−40563号)。しかし、この方法により得られる製剤は、糖や抗菌剤の安定性が悪く、満足できるものではなかった。
【0005】
このように、従来の糖を含有する製剤は、硬度が増したり、安定性に問題があるものであった。
従って、本発明の目的は、硬度変化が少なく、かつ安定な糖含有製剤を提供することにある。
【0006】
【課題を解決するための手段】
このような実状において、本発明者は鋭意研究を行った結果、平均粒子径の異なる粉末糖を2種以上配合することにより、硬度の経時変化が小さく、使用感が良い、安定な製剤が得られることを見出し、本発明を完成した。
【0007】
すなわち本発明は、平均粒子径の異なる粉末糖を2種以上配合したことを特徴とする損傷皮膚修復用半固形製剤を提供するものである。
【0008】
【発明の実施の形態】
本発明に用いられる粉末糖としては、例えば白糖(シュクロース)、グルコース、デキストロース、乳糖、マンニトール等が挙げられるが、日本薬局方の白糖又は精製白糖が品質の均一化のため好ましい。
【0009】
粉末糖の配合量は製剤全体の50〜90重量%(以下、単に「%」で示す)とすることが好ましく、特に60〜80%とすることが好ましい。
【0010】
粉末糖は、その平均粒子径が10μm〜1200μmの範囲のものが好ましく、特に10〜1000μmの範囲のものが好ましい。
【0011】
また、本発明においては平均粒子径の異なる粉末糖を2種以上配合することが必要であり、このような2種の組合せとしては、平均粒子径が10〜100μmの粉末糖と平均粒子径が150〜800μmのものとの組合せが好ましく、特に平均粒子径15〜80μmのものと平均粒子径が200〜400μmのものとの組合せが好ましく、これらの配合割合は1:1〜99:1が好ましく、特に2:1〜70:1が好ましく、更に4:1〜20:1が好ましい。
【0012】
本発明の製剤は、上記粉末糖以外に必要により、抗菌剤、保形剤、pH調整剤、可溶化剤、水等の1種又は2種以上を適宜組合せて配合することができる。
【0013】
抗菌剤としては、例えばポビドンヨード、塩酸クロルヘキシジン、塩化ベンザルコニウム、塩化ベンゼトニウム、セチルピリジニウムクロライド、イソプロピルメチルフェノール、硫酸ゲンタマイシン及びクロトリマゾール等が挙げられるが、ポビドンヨード、塩酸クロルヘキシジンが特に好ましい。抗菌剤の配合量は製剤全体の0.5〜10%とすることが好ましい。
【0014】
保形剤としては、例えば、デキストリン、アラビアゴム、プルラン、コンドロイチン硫酸、メチルセルロース、ヒドロキシメチルセルロース、カルボキシメチルセルロース等の多糖類又はその誘導体;ポリエチレングリコール400、1500、4000、6000、ポリオキシエチレンポリオキシプロピレングリコール、ポリプロピレングリコール等のグリコール類;グリセリン、ポリグリセリン等のグリセリン類;ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンポリオキシプロピレンブロックポリマー、ポリビニルピロリドン、ポリビニルアルコール、カルボキシビニルポリマー等が挙げられる。保形剤の配合量は製剤全体の10〜40%とするのが好ましい。
【0015】
pH調整剤としては、例えば塩酸、乳酸、クエン酸、リン酸、水酸化ナトリウム、水酸化カリウム、リン酸ナトリウム、フタル酸水素カリウム等が挙げられる。本製剤のpHは3.5〜6.0に調整することが好ましい。
可溶化剤としては、例えば、ヨウ化カリウム、ヨウ化ナトリウム、グリセリン等が挙げられる。可溶化剤の配合量は製剤全体の0.5〜30%とするのが好ましい。
水は、通常製剤に用いられる精製水を使用し、製剤全体の1〜30%使用することが好ましく、特に5〜20%使用することが好ましい。
【0016】
本発明の好ましい製剤としては、上記粉末糖を50〜90%、ポビドンヨードを0.5〜10%、及び水を1〜30%配合し、製剤のpHが3.5〜6に調整されたものが挙げられ、更に好ましい製剤としてはこれに保形剤を10〜40%及び/又は可溶化剤を0.5〜30%配合したものが挙げられる。
【0017】
本発明製剤の硬度は、後記試験例の測定条件のもとで120g以下が好ましく、特に100g以下が好ましい。
【0018】
本発明製剤の製造法は特に制限されないが、例えば、精製水にpH調整剤を加えて溶解した後、可溶化剤、抗菌剤及び保形剤を添加し、予め平均粒子径の異なる粉末糖を混合したものを添加し均一になるまで練合する方法が好ましい。
【0019】
【実施例】
次に実施例を挙げて説明するが、本発明はこれら実施例に限定されない。
【0020】
実施例1
下記表1の組成の損傷皮膚修復用半固形製剤を下記製法にて調製した。
【0021】
【表1】
(組成) (重量%)
(1)精製水 9.52
(2)クエン酸 0.1
(3)水酸化ナトリウム 0.08
(4)ポビドンヨード 3.0
(5)保形剤 17.3
(6)精製白糖(平均粒子径30μm) 63.0
(7)精製白糖(平均粒子径300μm) 7.0
【0022】
(製法)
(1)に(2)及び(3)を加えて溶解した溶液に、(4)を加え攪拌して溶解する。次に(5)を加えてよく攪拌した後、(6)及び(7)を添加しよく攪拌しながら練合し均一な製剤を得た。
【0023】
実施例2〜6、比較例1、2
下記表2に示す組成で、実施例1と同様にして製剤を調製した。
【0024】
試験例1
実施例1〜6及び比較例1、2の各製剤について、25℃で6ケ月間保存した時のザラザラ感、液の滲み、展延性及び硬度を評価した。その結果を表2に示す。
【0025】
硬度の測定方法
直径60mm、高さ55mmの容器に製剤100gを充填し、レオメーター(不動工業NRM−3002D−L)を用い25℃、Stroke 20mm、T.Speed 6cm/minの条件下で直径10mmの球形アダプターが、20mm侵入した時の負荷を測定した。
【0026】
【表2】
【0027】
試験例2
試験例1の硬度の測定方法により、各製剤の硬度の経時変化を測定した。その結果を図1に示す。
【0028】
上記試験例1及び2において、平均粒子径が30μmの粉末糖だけで調製した製剤は、調製後3ケ月で硬度が120g以上になり展延性が悪くなるため扱いにくくなった。また平均粒子径が300μmの粉末糖だけで調製した製剤は、調製後6ケ月の時点でも硬度は約40g以下で柔らかいが、ザラつきがある為使用感が悪く、また液の滲みも認められた。
【0029】
【発明の効果】
本発明の損傷皮膚修復用半固形製剤は、硬度の経時変化が少なく、安定で長期間良好な使用感を保持する。
【図面の簡単な説明】
【図1】各製剤の硬度の経時変化を示す図である。[0001]
BACKGROUND OF THE INVENTION
The present invention relates to a semi-solid preparation for damaged skin repair, which contains powdered sugar, has a small change in hardness over time, is stable, and maintains a good feeling for a long period of time.
[0002]
[Prior art]
Since sugar has a wound healing action and granulation action, it is used for the treatment of burns and open wounds. In recent years, preparations obtained by adding antibacterial agents such as povidone iodine to sugar have been used as preparations for repairing damaged skin [RA Knutson et. Al .; Southern Medical Journal, Vol. 74, No. 11, 1329-1335. (1981) and Kiyokazu Sone et al., “Hospital Pharmacy”, Vol. 10, No. 5, 315-322 (1984)].
[0003]
[Problems to be solved by the invention]
However, such a sugar-containing preparation has a problem that the hardness increases with time after preparation. The increase in hardness deteriorates the spreadability and makes it difficult to apply to the scratched part. In addition, the sugar-containing preparations have a problem that the uniformity is lost over time, resulting in a rough feeling of use.
[0004]
As a method for reducing the hardness of a sugar-containing preparation, there are methods of decreasing the amount of sugar and increasing the amount of water, but any of these methods may cause liquid bleeding or spots on the upper or lower layer of the preparation. Appeared, and there was a problem in stability.
Recently, a method of blending a high concentration of glycerin to improve the extensibility of a sugar-containing preparation has been reported (Japanese Patent Laid-Open No. 9-40563). However, the preparation obtained by this method is not satisfactory because of the poor stability of sugars and antibacterial agents.
[0005]
Thus, conventional sugar-containing preparations have increased hardness and have problems with stability.
Accordingly, an object of the present invention is to provide a stable sugar-containing preparation with little change in hardness.
[0006]
[Means for Solving the Problems]
In such an actual situation, as a result of intensive studies, the present inventor has obtained a stable preparation with a small change in hardness over time and good usability by blending two or more powdered sugars having different average particle sizes. The present invention has been completed.
[0007]
That is, the present invention provides a semi-solid preparation for repairing damaged skin, wherein two or more powdered sugars having different average particle diameters are blended.
[0008]
DETAILED DESCRIPTION OF THE INVENTION
Examples of the powdered sugar used in the present invention include sucrose, glucose, dextrose, lactose, mannitol, and the like. Japanese pharmacopoeia saccharose or purified sucrose is preferred for uniform quality.
[0009]
The blending amount of the powdered sugar is preferably 50 to 90% by weight (hereinafter simply referred to as “%”) of the whole preparation, particularly preferably 60 to 80%.
[0010]
The powdered sugar preferably has an average particle size in the range of 10 μm to 1200 μm, particularly preferably in the range of 10 to 1000 μm.
[0011]
In the present invention, it is necessary to blend two or more kinds of powdered sugars having different average particle diameters. Such two kinds of combinations include powdered sugars having an average particle diameter of 10 to 100 μm and an average particle diameter. A combination of those having an average particle size of 15 to 80 μm and a combination of those having an average particle size of 200 to 400 μm is preferable, and the mixing ratio thereof is preferably 1: 1 to 99: 1. In particular, 2: 1 to 70: 1 is preferable, and 4: 1 to 20: 1 is more preferable.
[0012]
In addition to the powdered sugar, the preparation of the present invention may contain one or two or more of antibacterial agents, shape-retaining agents, pH adjusters, solubilizers, water and the like as necessary.
[0013]
Examples of the antibacterial agent include povidone iodine, chlorhexidine hydrochloride, benzalkonium chloride, benzethonium chloride, cetylpyridinium chloride, isopropylmethylphenol, gentamicin sulfate, and clotrimazole, with povidone iodine and chlorhexidine hydrochloride being particularly preferable. The blending amount of the antibacterial agent is preferably 0.5 to 10% of the whole preparation.
[0014]
Examples of the shape-retaining agent include polysaccharides such as dextrin, gum arabic, pullulan, chondroitin sulfate, methyl cellulose, hydroxymethyl cellulose, carboxymethyl cellulose, and derivatives thereof; polyethylene glycol 400, 1500, 4000, 6000, polyoxyethylene polyoxypropylene glycol And glycols such as polypropylene glycol; glycerins such as glycerin and polyglycerin; polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene block polymer, polyvinylpyrrolidone, polyvinyl alcohol, carboxyvinyl polymer, and the like. The amount of the shape-retaining agent is preferably 10 to 40% of the whole preparation.
[0015]
Examples of the pH adjuster include hydrochloric acid, lactic acid, citric acid, phosphoric acid, sodium hydroxide, potassium hydroxide, sodium phosphate, potassium hydrogen phthalate and the like. The pH of this preparation is preferably adjusted to 3.5 to 6.0.
Examples of the solubilizer include potassium iodide, sodium iodide, glycerin and the like. The blending amount of the solubilizer is preferably 0.5 to 30% of the whole preparation.
As the water, purified water usually used for preparations is used, preferably 1 to 30%, more preferably 5 to 20% of the whole preparation.
[0016]
As a preferable preparation of the present invention, 50 to 90% of the above powdered sugar, 0.5 to 10% of povidone iodine, and 1 to 30% of water are mixed, and the pH of the preparation is adjusted to 3.5 to 6 More preferable preparations include those containing 10 to 40% of a shape-retaining agent and / or 0.5 to 30% of a solubilizer.
[0017]
The hardness of the preparation of the present invention is preferably 120 g or less, particularly preferably 100 g or less, under the measurement conditions described later in Test Examples.
[0018]
The production method of the preparation of the present invention is not particularly limited. For example, after adding a pH adjuster to purified water and dissolving, a solubilizer, an antibacterial agent and a shape-retaining agent are added, and powdered sugars having different average particle sizes are previously added. A method of adding a mixture and kneading until uniform is preferable.
[0019]
【Example】
Next, although an example is given and explained, the present invention is not limited to these examples.
[0020]
Example 1
A semi-solid preparation for repairing damaged skin having the composition shown in Table 1 below was prepared by the following method.
[0021]
[Table 1]
(Composition) (wt%)
(1) Purified water 9.52
(2) Citric acid 0.1
(3) Sodium hydroxide 0.08
(4) Povidone iodine 3.0
(5) Shape retention agent 17.3
(6) Purified sucrose (average particle size 30 μm) 63.0
(7) Purified sucrose (average particle size 300 μm) 7.0
[0022]
(Manufacturing method)
(4) is added to the solution obtained by adding (2) and (3) to (1) and dissolved, and dissolved by stirring. Next, (5) was added and stirred well, then (6) and (7) were added and kneaded with good stirring to obtain a uniform preparation.
[0023]
Examples 2 to 6, Comparative Examples 1 and 2
A formulation having the composition shown in Table 2 below was prepared in the same manner as in Example 1.
[0024]
Test example 1
About each formulation of Examples 1-6 and Comparative Examples 1 and 2, the rough feeling, the oozing of a liquid, spreadability, and hardness when preserve | saved at 25 degreeC for 6 months were evaluated. The results are shown in Table 2.
[0025]
Method for measuring hardness 100 g of the preparation was filled in a container having a diameter of 60 mm and a height of 55 mm, and a rheometer (Fudo Kogyo NRM-3002D-L) was used at 25 ° C., Stroke 20 mm, T.P. A load was measured when a spherical adapter having a diameter of 10 mm invaded 20 mm under a speed of 6 cm / min.
[0026]
[Table 2]
[0027]
Test example 2
With the hardness measurement method of Test Example 1, the change with time of the hardness of each preparation was measured. The result is shown in FIG.
[0028]
In Test Examples 1 and 2, the preparation prepared only with powdered sugar having an average particle size of 30 μm became difficult to handle because the hardness became 120 g or more in 3 months after preparation and the spreadability deteriorated. In addition, the preparation prepared only with powdered sugar having an average particle size of 300 μm had a hardness of about 40 g or less even at the time of 6 months after preparation, but it had a rough feel and the feeling of use was poor, and liquid bleeding was also observed. .
[0029]
【The invention's effect】
The semi-solid preparation for repairing damaged skin of the present invention has little change over time in hardness, and is stable and maintains a good feeling for a long time.
[Brief description of the drawings]
BRIEF DESCRIPTION OF DRAWINGS FIG. 1 is a graph showing changes in hardness of each preparation over time.
Claims (3)
Priority Applications (1)
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JP33539297A JP4116687B2 (en) | 1997-12-05 | 1997-12-05 | Semi-solid preparation for damaged skin repair |
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JP33539297A JP4116687B2 (en) | 1997-12-05 | 1997-12-05 | Semi-solid preparation for damaged skin repair |
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JPH11171779A JPH11171779A (en) | 1999-06-29 |
JP4116687B2 true JP4116687B2 (en) | 2008-07-09 |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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KR20180011882A (en) * | 2015-01-20 | 2018-02-02 | 벨로체 바이오파르마 엘엘씨 | Novel iodophor composition and methods of use |
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
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KR20180011882A (en) * | 2015-01-20 | 2018-02-02 | 벨로체 바이오파르마 엘엘씨 | Novel iodophor composition and methods of use |
KR20180011883A (en) * | 2015-01-20 | 2018-02-02 | 벨로체 바이오파르마 엘엘씨 | Novel iodophor composition and methods of use |
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